Effects of brotizolam on smooth muscle and other organs

Effects of brotizolam (2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-1,2,4-triazolo [4,3-a]-1,4-diazepine, We 941, Lendormin) on smooth muscle and other biological systems were examined. In isolated intestinal preparations, brotizolam in higher concentrations shifted the concentration-contractile response curve after addition of acetylcholine down to the right. However, brotizolam did not affect the intestinal transport. Therefore, even if brotizolam possesses a non-specific inhibitory action on smooth muscle, it would be quite weak. Brotizolam, nitrazepam and estazolam in high doses showed a miotic action. Brotizolam had no effect on the digestive system, that is, gastric secretion, bile secretion and intestinal propulsive activity were not influenced. A depression of salivary secretion, which may be due to an additive action of Eidelberg's mixture, was observed. Brotizolam, nitrazepam and estazolam enhanced the sleeping time induced by ethanol and increased locomotor activity induced by methamphetamine, but did not affect the chewing behavior. There was no indication that continuous administration of brotizolam affected significantly the levels of lipids and sugar in the blood serum.